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24 Cards in this Set
- Front
- Back
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As the concentration of free ligand increases (more/less) ligand binds to receptor
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more
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water is a p_____ molecule
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polar
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Asymmetric distribution of the electron cloud results in the formation of a....
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temporary dipole
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What are radioligands?
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Compounds where 1 or more atoms have been replaced by a radioactive alternative
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What is the usual radioligand?
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tritium3H
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Radioligand (does/does not) affect ligand structure and binding
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does not
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Radioligands can be both agonist or antagonist but generally they tend to be _________
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antagonist
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If the G protein-coupled receptor is GDP bound then binding of agonist is (high/low)
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high
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If the G protein-coupled receptor is GTP bound then binding of agonist is (high/low)
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low
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If the G protein-coupled receptor is GDP bound then binding of antagonist is (high/low)
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high
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If the G protein-coupled receptor is GTP bound then binding of antagonist is (high/low)
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high
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To calculate Bmax and Kd what other 2 curve must be drawn?
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non-selective binding
specific binding |
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What are the axis to calculate Bmax and Kd?
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Bound (moles/mg) - y-axis
Concentration of free (M) - x-axis |
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For a scatchard plot how do we calculate the gradient
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gradient = 1/Kd
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On a scatchard plot the intercept on the x-axis is...
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Bmax
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What are the axis on a scatchard plot
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Bound/free(y-axis) and Bound (x-axis)
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The competition binding experiment uses ____ ligands
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2
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What is the principle for the competition binding experiment?
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to compete off the radiolabelled with the non-radiolabelled drug
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What 2 things must remain constant in the competition binding experiment?
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Radiolabelled ligand
Protein |
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The first step to competition binding experiment is to __________ receptor with a concentration of radiolabelled drug (above/below) its Kd
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incubate
below |
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The second step to the competition binding experiment is to ___ increasing concentration of non-labelled drug
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add
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What does the IC50 represent?
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Concentration of competitor required to displace 50% of the radioligand
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The third step to the competition binding experiment is to draw a graph to calculate _____
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IC50
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What is the Cheng Prusoff equation?
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Kd(competitor) = IC50/1+(concentration of radioligand/Kd(radioligand))
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